Methadone

Profile

Methadone is a synthetic, narcotic
analgesic (pain reliever). Often used by and associated with the treatment of
heroin addicts it is also used
for other medical purposes such as pain relief. The drug shares many of the
same effects and characteristics of morphine and acts in similar ways to it
and other narcotic medications. However, with methadone the gradual and mild
onset of action prevents the user from getting high and experiencing euphoric
effects.1 Doses used in
heroin treatment vary based
on a person's body weight and opiate tolerance; but proper dosage is measured
and determined by a patients decline in opiate cravings. Despite its use in
the treatment community, there are addicts who use methadone as their primary
drug of choice. Supplies of the drug for these users are illegal and are diverted
from legitimate methadone programs by enrolled methadone patients.2
In 2000, there were an estimated 1,200 treatment facilities in the U.S. dispensing
methadone.3 The drug is currently a
Schedule II and is
available in oral solutions, tablets, and injectable forms.4
And although there is no one manufacturer responsible for producing methadone,
the active ingredient is always the same: methadone hydrochloride.5
Still, methadone is frequently encountered on the illicit market and has been
associated with a growing number of overdose deaths.6, 7

History

The chemical structure of methadone was first produced in the 1930's as a
team of German scientists was searching for a pain-killing drug (analgesic)
that would not be as addictive as morphine. In 1937, two scientists
(Max Bockmhl and Gustav Ehrhart) uncovered a synthetic substance that they
called Hoechst 10820 or polamidon. Years later during World War II another
team of German scientists expanded on earlier research and began synthesizing
the substance as a result of short supplies of morphine and other
analgesics.8 By the end of the war, the United
States had obtained the rights to the drug from war requisitions and later
coined the name methadone.9 Soon after in 1947
methadone was introduced into the United States to be used as a pain reliever
for a variety of conditions, but eventually uncovered its usefulness in
treating narcotic addictions.10 Until the
1960's, little scientific advancement was made with regard to methadone.
But with a resurgence of heroin addiction, researchers began to search for
a substance that could reduce or eliminate drug craving and
withdrawal signs and
symptoms.11 The idea behind this research was
that methadone could be used to manage or maintain heroin
addiction. In 1964,
the effectiveness and usefulness of using methadone maintenance (i.e., using it
as a substitute narcotic to prevent withdrawal) was realized. In the spring of
1971, methadone treatment for opiate dependence began to expand. That year
the Federal Government developed regulations governing the use of methadone in
the treatment of heroin addiction; final regulations were published in December
1972. Few advancements were made until 2001 when regulations over methadone
were modified to allow physicians and other health care professionals to provide
methadone more effectively and consistently.12

Methods of Use

Methadone is dispensed primarily in oral forms, including tablets, powder,
and liquid for the treatment of narcotics addiction. Single doses, which
should not exceed 80 - 100 milligrams daily, can last anywhere from 24 to
36 hours depending on user characteristics (e.g., age, weight, level of
addiction, and tolerance); the long-acting nature of the drug is a distinct
advantage since it requires less frequent administration, limiting potential
harmful effects.13 Tablet forms of the drug,
sometimes called diskettes, contain approximately 40 milligrams of methadone
and are often dissolved in water and ingested orally. There is also a white
crystalline powder form available that is dissolved in water and swallowed.
Finally, liquid is sometimes used in treatment clinics; with this method dosages
of methadone can be tightly controlled and adjusted to as small as one milligram,
this allows patients to receive just the right amount of methadone needed to
curb their withdrawal symptoms.14 Illicit
methadone is sometimes administered through injection (injection is not a
valid route of administration in treatment) directly into the bloodstream.
This form subjects users to increased risks of a variety of diseases, including
HIV/AIDS.

Physical Effects

Though methadone is primarily used for treating narcotics
addiction,
users can still experience negative physical effects. Careful monitoring
and a close relationship between a doctor and the patient are essential
to its proper use.15 Reinforcing effects
of methadone are limited, as the drug is designed to block the pleasurable
effects of opiates, but only when administered in the correct dosage(s).
Some of the physical and side effects of methadone are:

Methadone Maintenance

First appearing in Canada, methadone maintenance programs in the U.S.
are often thought about as one of the most common and effective means
for treating heroin
addiction16;
in the late 1970's they gained considerable acceptance and already had
more than 75,000 participants.17
The term "maintenance" is used in describing these programs because
the goal is to "maintain" a narcotics abuser for the purpose of helping
him or her avoid the negative and sometimes severe withdrawal
symptoms.18 This type of treatment views
addiction as a disease rather than a psychological disorder or character
flaw.19 A number of studies have looked
at the effectiveness of methadone programs, and a majority of them have
found that methadone can reduce narcotics related deaths, heroin users'
involvement in crime, the spread of AIDS, and also help users gain control
of their lives.20

Addiction, Tolerance,
Withdrawal, and Dependence

Although methadone is intended to prevent narcotics addiction and
dependence along with associated withdrawal symptoms, there is still
the possibility of becoming addicted. In fact methadone is an extremely
physically addictive drug; however addiction is less likely when under
the supervision of a doctor.21
Tolerance to methadone can also occur with frequent administration,
though studies have shown that a user's tolerance may not increase if
prescribed correctly.22 Withdrawal symptoms
occurring from the use of methadone are not as common as they are with
heroin; therefore it is possible to maintain an addict on methadone
without certain harsh side effects.23
Psychological and physical dependence can develop with the use of
methadone.24 For instance, use of the drug
continues a user's opioid dependency, but frees them from uncontrolled,
compulsive, and disruptive behavior associated with heroin
addiction.25

Alternatives to Methadone

Aside from methadone, there are currently at least two alternative options
for the treatment of opioid dependence: Bupernorphine and LAAM. But it
is still important to remember that outside of a doctor's care these drugs
can be equally as addictive as methadone, resulting in dependence, tolerance,
and withdrawal.

Bupernorphine

Bupernorphine is a potent (30-50 times greater than morphine) semi-synthetic
narcotic substance that has recently been approved (after 12 years of
extensive research) to help treat heroin and opioid
dependency.26 First developed in the late 1970's,
Bupernorphine is currently available in the United States as an injectable
Schedule V narcotic analgesic (Buprenex) for human and veterinary
use 27 (tablet forms are also available).
Unlike the other treatment drugs, Bupernorphine produces far less respiratory
depression and is thought to be safer in the event of an overdose. In addition,
it does not produce significant levels of physical dependence or discomforting
withdrawal symptoms; so discontinued use is easier than methadone.

LAAM

In 1994 the FDA approved L-alpha-acetyl-methadol (LAAM) as a Schedule II drug
for use in treatment of addiction.28 LAAM may
be used instead of methadone because it has longer lasting effects, and instead
of daily visits to treatment, addicts may only need to take the drug three
times a week.29 Considered safe and effective,
this drug is available primarily in oral forms such as pills and tablets.
Like methadone, LAAM does not produce euphoric effects; however, because most
patients are not familiar with LAAM, they may be initially more anxious and
need more counseling and support when receiving the medication than they
would with methadone.30 In addition to anxiety,
users are subjected to a number of side effects such as: abnormal liver
functioning, rashes, nausea, and increased blood
pressure.31